Objective: To encapsulate ginsenoside Rh2 within glycyrrhetinic acid modified liposomes and investigate its physicochemical properties and in vitro inhibitory effect on SMMC-7721 cells. Method: Ginsenoside Rh2 liposomes(Rh2-L) and ginsenoside Rh2 liposomes surface-modified with glycyrrhetinic acid(GA-Rh2-L) were prepared by film dispersion method

UPLC was employed to determine the content of ginsenoside Rh2 with mobile phase of acetonitrile-water(28: 72)

flow rate of 0.3 mL·min-1 and detection wavelength at 203 nm.Encapsulation efficiency(EE)

particle size

Zeta potential and in vitro release were measured

MTT experiment was adopted to evaluate inhibitory effect of ginsenoside Rh2 solution

Rh2-L and GA-Rh2-L on SMMC-7721 cells. Result: Modification of glycyrrhetinic acid showed no effect on physicochemical properties of Rh2-L

such as EE

particle size

Zeta potential and in vitro release.EE of Rh2-L and GA-Rh2-L were (91.67±1.05)% and (95.54±2.23)%

average particle size of them were (138.6±45.8) nm and (146.5±48.9) nm

Zeta potential of them were -(12.75±0.34) mV and -(14.79±0.67) mV

respectively.In vitro release of ginsenoside Rh2 from Rh2-L and GA-Rh2-L within 72 h were (84.67±7.23)% and (89.03±8.61)%

while ginsenoside Rh2 solution released (91.23±5.17)% within 12 h.In vitro cytotoxicities(IC50) of GA-Rh2-L on SMMC-7721 cells was increased by 0.524 fold compared with ginsenoside Rh2 solution and 0.596 fold compared with Rh2-L.Ginsenoside Rh2 solution

Rh2-L and GA-Rh2-L all inhibited proliferation of SMMC-7721 cells in dose-and-time-dependent manners. Conclusion: Glycyrrhetinic acid modification can not affect physicochemical properties of Rh2-L

and it can increase targeting efficiency of liposomes on hepatocellular carcinoma

thus resulting in higher cytotoxicities in comparison with Rh2-L.This study provides new ideas for targeted-therapy to hepatocellular carcinoma.